SYNTHESIS AND BIOLOGICAL EVALUATION OF 2-SUBSTITUTED PHENYL-1-(SUBSTITUTED PIPERAZIN-1-YL) METHYL)-1H-BENZO[D]IMIDAZOLES

INDIAN DRUGS ◽  
2013 ◽  
Vol 50 (01) ◽  
pp. 50-58
Author(s):  
S. K Gupta ◽  
◽  
N. Kumar ◽  
D. Pathak
Keyword(s):  
Antibacterial Activity ◽  
Anthelmintic Activity ◽  
Mannich Bases ◽  
Biological Evaluation ◽  
Biologically Active ◽  
Diffusion Method ◽  
Benzimidazole Derivatives ◽  
Bacterial Strains ◽  
Death Time ◽  
Synthesis And Biological Evaluation

A series of biologically active benzimidazole derivatives (2a-2n) was synthesized by the reaction of o-phenylenediamine with the derivatives of benzoic acid in presence of 4N-HCl followed by the reaction with piperazine and formaldehyde to undergo Mannich reaction. The structures of all the synthesized Mannich bases were characterized by UV, FTIR, 1H NMR, mass spectroscopy and elemental analysis. The compounds were evaluated for their anthelmintic activity by the identification of paralyzing and death time by using mebendazole as standard in the concentration of 2 mg/ml. The compounds 2a, 2b, 2e and 2h were found to be most potent for anthelmintic activity. All the compounds were also evaluated for antibacterial activity against gram-positive bacterial strains like Bacillus subtilis and Streptococcus aureus, and gram-negative bacterial strains like Escherichia coli and Pseudomonas aeruginosa. The study was performed through disc diffusion method by using Ciprofloxacin as standard in the concentration of 50µg/ml. The compounds 2e, 2h, 2k, 2l and 2m were found to possess significant antibacterial activity.

scholarly journals Synthesis and biological evaluation of some new 7H-[1,2,4]triazolo[3,4-b][1,3,4]thiadiazines as antimicrobial agents

2022 ◽  
Vol 11 (1) ◽  
pp. 75-82 ◽  
Author(s):  
Iryna Myrko ◽  
Taras Chaban ◽  
Vasyl Matiychuk
Keyword(s):  
Mass Spectrometry ◽  
Escherichia Coli ◽  
Staphylococcus Aureus ◽  
Pseudomonas Aeruginosa ◽  
Antimicrobial Activity ◽  
Antibacterial Activity ◽  
Antimicrobial Agents ◽  
Biological Evaluation ◽  
Bacterial Strains ◽  
Synthesis And Biological Evaluation

A series of some new pyrazole-substituted 7H-[1,2,4]triazolo[3,4-b][1,3,4]thiadiazines was synthesized in this study. The structures of target substances were confirmed by using 1H and 13С NMR spectroscopy, mass spectrometry and elemental analysis. The synthesized compounds have been evaluated for antimicrobial activity against five bacterial strains (Escherichia coli, Klebsiella pneumoniae, Acinetobacter baumannii, Pseudomonas aeruginosa, Staphylococcus aureus) and two fungal strains (Candida albicans and Cryptococcus neoformans). The antimicrobial screening studies of synthesized substances established that 2 of 12 compounds show pronounced antibacterial activity against the strain Staphylococcus aureus.

SYNTHESIS AND EVALUATION OF ANTIBACTERIAL, ANTHELMINTIC ACTIVITIES OF SUBSTITUTED BENZIMIDAZOLE DERIVATIVES

INDIAN DRUGS ◽  
2017 ◽  
Vol 54 (06) ◽  
pp. 69-76
Author(s):  
D Sharma ◽  
◽  
G. K Sharma ◽  
D. Pathak ◽  
M. C. Sharma
Keyword(s):  
Antibacterial Activity ◽  
Anthelmintic Activity ◽  
Benzimidazole Derivatives ◽  
The Novel ◽  
Bacterial Strains ◽  
Gram Positive ◽  
Alkyl Aryl ◽  
Gram Negative ◽  
E Coli

The study was undertaken to synthesize and evaluate antibacterial, anthelmintic activities of N’ (substituted benzylidene)-2-(2-alkyl/aryl-1H-benzo[d] imidazole-1yl) acetohydrazide derivatives. All the novel benzimidazole derivatives were screened for anthelmintic activity against Pherituma posthuma species of earthworms and antibacterial activity against following bacterial strains: S. aureus, B.subtilis (Gram positive) and E. coli and P.aeruginosa (Gram negative). The antibacterial data suggest that compounds having nitro and hydroxyl substitution were more potent and the anthelmintic data suggest that compounds having chloro were most active.

scholarly journals Synthesis and biological evaluation of new hydrazide-Schiff bases

2015 ◽  
Vol 10 (3) ◽  
pp. 555 ◽  
Author(s):  
Asif Husain ◽  
Munendra M. Varshney ◽  
Versha Parcha ◽  
Aftab Ahmad ◽  
Shah Alam Khan
Keyword(s):  
Schiff Bases ◽  
Anthelmintic Activity ◽  
Biological Evaluation ◽  
Gram Negative Bacteria ◽  
Bacterial Strains ◽  
E Coli ◽  
New Class ◽  
Antibacterial Screening ◽  
Synthesis And Biological Evaluation

<div><p>A new series of N-({5-(substituted aryl)-furan-2-yl}-methylidene)-hydrazides were synthesized with a new class of Schiff bases derived from the reaction of substituted phenyl-1-ketohydrazide <strong>2</strong> or 2-(4-chloro-3-methylaryloxy) acetohydrazide <strong>3</strong> with different 5-(substituted aryl)-2-furfuraldehyde (<strong>1a-k</strong>) to yield substituted N-({5-(substituted aryl)-furan-2-yl}-methylidene)-hydrazides-Schiff bases <strong>(4a-f, 4g-k)</strong>. The title compounds were subjected to <em>in vitro</em> antibacterial screening against Gram positive bacterial strains-<em> S. aureus</em>, <em>B. cereus</em>, <em>E. faecalis</em> and <em>S. epidermidis</em>, and Gram negative bacteria strains- <em>E. coli</em>, <em>S. typhi</em>, <em>S. dysenteriae</em>  and <em>K. pneumoniae</em>. The synthesized Schiff bases were also evaluated for their anthelmintic activity against two species of earthworms (<em>Pheritima posthuma</em> and <em>Perionyx excavates</em>). Some compounds have shown promising antibacterial and anthelmintic activities.</p></div>

scholarly journals Synthesis and Biological Evaluation of Some Piperazine Derivatives as Anti-Inflammatory Agents

2019 ◽  
Vol 9 (4-s) ◽  
pp. 353-358
Author(s):  
Nalini Patel ◽  
Vaishali Karkhanis ◽  
Pinkal Patel
Keyword(s):  
Mannich Bases ◽  
Biological Evaluation ◽  
Benzimidazole Derivatives ◽  
Piperazine Derivatives ◽  
Rat Paw Edema ◽  
In Series ◽  
Anti Inflammatory ◽  
Rat Paw ◽  
Synthesis And Biological Evaluation

Some 1-((4-methylpiperazin-1yl)methyl)-1H-benzo[d]imidazole & 1-((4-phenylpiperazin-1yl)methyl)-1H-benzo[d]imidazole derivatives were synthesized through reaction of 1-substituted piperazines with different benzimidazole derivatives in methanol yielded the corresponding mannich bases (42-a to 42-i). All the synthesized compounds were elucidated by IR, 1H NMR and MASS spectroscopy. They were tested for anti-inflammatory activity using in-vivo (Carrageenan- induced rat paw edema model) method at a dose of 50mg/kg. result showed that compounds 42-c, 42-d and 42-h were found to be most potent in series. Keywords: 1,4-disubstituted Piperazine, Anti-inflammatory, Mannich Base.

scholarly journals Synthesis and Biological Evaluation of 7-O-Modified Formononetin Derivatives

2008 ◽  
Vol 2008 ◽  
pp. 1-4 ◽  
Author(s):  
Ying Yang ◽  
Wen-Jun Mao ◽  
Huan-Qiu Li ◽  
Tao-Tao Zhu ◽  
Lei Shi ◽  
...  
Keyword(s):  
Antibacterial Activity ◽  
Cell Line ◽  
Jurkat Cell ◽  
Preliminary Investigation ◽  
Biological Evaluation ◽  
Bacterial Strains ◽  
Chemical Structures ◽  
Structure Activity ◽  
Synthesis And Biological Evaluation ◽  
Antiproliferative Activities

Three series of novel formononetin derivatives were synthesized, in which formononetin and heterocyclic moieties were separated by 2-carbon, 3-carbon, and 4-carbon spacers. The chemical structures of these compounds were confirmed. All the derivatives were screened for antiproliferative activities against Jurkat cell line and HepG-2 cell line. In this paper, compounds prepared were also screened for their antibacterial activity of six bacterial strains. Compound 3b exihibited promising antibacterial activity against B. subtilis with minimal inhibitory concentration (MIC) value of 0.78 μg/mL, and compound 5e showed significant antiproliferative activities against Jurkat cell growth with IC50 of 1.35×10−4 μg/mL. The preliminary investigation of structure-activity relationships (SARs) was also discussed based on the obtained experimental data.

ChemInform Abstract: Synthesis and Biological Evaluation of Mannich Bases of Benzimidazole Derivatives.

ChemInform ◽  
2011 ◽  
Vol 43 (4) ◽  
pp. no-no
Author(s):  
G. Mariappan ◽  
N. R. Bhuyan ◽  
Pradep Kumar ◽  
Deepak Kumar ◽  
K. Murali
Keyword(s):  
Mannich Bases ◽  
Biological Evaluation ◽  
Benzimidazole Derivatives ◽  
Synthesis And Biological Evaluation

Synthesis and Biological Evaluation of Benzothiazole-piperazinesulfonamide Conjugates and Their Antibacterial and Antiacetylcholinesterase Activity

2019 ◽  
Vol 16 (9) ◽  
pp. 723-734
Author(s):  
B. Ramalingeswara Rao ◽  
Mohana R. Katiki ◽  
Kommula Dileep ◽  
C. Ganesh Kumar ◽  
G. Narender Reddy ◽  
...  
Keyword(s):  
Antibacterial Activity ◽  
Inhibitory Activity ◽  
Micrococcus Luteus ◽  
Antimicrobial Activities ◽  
Biological Evaluation ◽  
Bacterial Strains ◽  
Reference Drug ◽  
Ache Inhibitory Activity ◽  
Synthesis And Biological Evaluation

Two series of N-2-benzothiazolyl-4-(arylsulfonyl)-1-piperazineacetamides/propanamides were synthesized from substituted 2-aminobenzothiazoles and were assayed for their in vitro antimicrobial activities against a panel of different pathogenic bacterial strains such as Micrococcus luteus, S. aureus, S. aureus MLS-16, B. subtilis, Escherichia coli, Pseudomonas aeruginosa, Klebsiella planticola and Candida albicans. Among the synthesized compounds 5e,f,g and 6g,h,i showed promising antifungal activity against C. albicans as compared to the reference drug, miconazole. Further, compounds 6g,h,i showed broad spectrum antibacterial activity against all the tested bacterial strains, while the compounds 6a-f,j-m showed significant antibacterial activity against all the tested bacterial strains as compared to the reference drug, ciprofloxacin. In addition, the target compounds were evaluated for their acetylcholinesterase (AChE) inhibitory activity, and, among the tested, compounds 5j,k,l and 6i showed promising AChE inhibitory activity.

scholarly journals Synergistic antibacterial activity of herbal extracts with antibiotics on bacteria responsible for periodontitis

2021 ◽  
Vol 15 (11) ◽  
pp. 1685-1693
Author(s):  
Shahabe Abullais Saquib ◽  
Nabeeh Abdullah AlQahtani ◽  
Irfan Ahmad ◽  
Suraj Arora ◽  
Shaik Mohammed Asif ◽  
...  
Keyword(s):  
Antibacterial Activity ◽  
Plant Extracts ◽  
Bacterial Resistance ◽  
Antibacterial Effect ◽  
Punica Granatum ◽  
Biologically Active ◽  
Diffusion Method ◽  
Bacterial Strains ◽  
Periodontopathic Bacteria ◽  
Favorable Conditions

Introduction: Development of bacterial resistance and antimicrobial side-effect has shifted the focus of research toward Ethnopharmacology. A biologically active compound derived from the plants may increase the effectiveness of antibiotic when used in combination. The present study aims to determine the synergistic antibacterial effect of ethanolic extracts of Punica granatum (pericarp), Commiphora molmol, Azadirachta indica (bark) in combination with amoxicillin, metronidazole, tetracycline, and azithromycin on periodontopathic bacteria: Porphyromonas gingivalis, Tannerella forsythia, Treponema denticola and Aggregatibacter actinomycetemcomitans. Methodology: Periodontopathic bacterial strains were isolated from the plaque sample that was collected from periodontitis patients and grown under favorable conditions. Susceptibility of bacteria to the antibiotics and extracts was determined by disc diffusion method by measuring the diameter of the inhibition zones. Minimum inhibitory concentration (MIC) and minimum bactericidal concentration (MBC) of plant extracts were evaluated against each bacterium. Synergistic effect of plant extract in combination with antibiotics was tested against each bacterium by measuring the diameter of zone of inhibition (ZOI). Results: Findings revealed that all plant extracts exhibited an inhibitory effects on the proliferation and growth of periodontopathic bacteria. The maximum antibacterial effect was exhibited by C. molmol on P. gingivalis (ZOI = 20 ± 0.55 mm, MIC = 0.53 ± 0.24 mg/mL and MBC = 5.21 ± 1.81 mg/mL) (p < 0.05), meanwhile, no antibacterial activity was exhibited by P. granatum on T. forsythia. Synergistic antibacterial effect was recorded when plant extracts were used in combination with antibiotics. The best synergism was exhibited by P. granatum with amoxicillin against A. actinomycetemcomitans (24 ± 1.00 mm) (p < 0.05). Conclusions: The synergistic test showed significant antibacterial activity when plant extracts were combined with antibiotics against all the experimented bacteria.

Synthesis, Characterization and Biological Evaluation of Cyclic Peptides: Viscumamide, Yunnanin A and Evolidine

2005 ◽  
Vol 60 (12) ◽  
pp. 1313-1320 ◽  
Author(s):  
Boja Poojary ◽  
S. L. Belagali
Keyword(s):  
Growth Inhibition ◽  
Spectral Data ◽  
Cyclic Peptides ◽  
Anthelmintic Activity ◽  
Biological Evaluation ◽  
Biologically Active ◽  
Bacterial Strains ◽  
Mass Spectral Data ◽  
Pharmacological Activities ◽  
Mass Spectral

Three biologically active cyclic peptides, viscumamide, yunnanin A and evolidine were synthesized and the structures were established on the basis of analytical, IR, NMR and mass spectral data. These newly synthesized cyclic peptides were evaluated for antimicrobial and pharmacological activities. Evolidine showed better growth inhibition against bacterial strains than yunnanin A and viscumamide. The anti-inflammatory activity of viscumamide is moderate and the remaining two cyclic peptides are found to be less active. But, all the three cyclic peptides showed weak anthelmintic activity.

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